Pharmacological characterization of β-adrenoceptor subtypes
| β1 | β2 | β3 | β4(?) | |
|---|---|---|---|---|
| Potency order | ISO > E = NE | ISO > E > NE | ISO = NE > E | ? |
| Selective agonists | NE3-a | Terbutaline | CGP 121773-c | CGP 121773-c |
| Xamoterol3-a 3-b | Salbutamol | CL 3162433-d | RO 363 (μM) | |
| RO 363 (nM)3-a 3-b | Procaterol | BRL 373443-d | ||
| Fenoterol | ||||
| Zinterol | ||||
| Selective antagonists | CGP 20712A (8.5–9.3) | ICI 118,551 | Bupranolol3-c | Bupranolol3-c |
| Betaxol (8.5) | (8.3–9.2) | (6.9–7.3) | (6.4–7.3) | |
| Atenolol (7.6) | SR 59230A | |||
| Bisoprolol (8.1–8.8) | (7.5–8.8) |
ISO, isoprenaline; NE, noradrenaline; E, adrenaline. Drug affinities (numbers in parentheses) are expressed as −logK i or −log K B values. Adapted from Alexander and Peters (1999), Bylund et al. (1998), Brodde (1997),Kaumann and Molenaar (1997), Manara et al. (1996), Molenaar et al. (1997).
↵3-a Selective relative to β2-adrenoceptors.
↵3-b In some tissues, partial agonists.
↵3-c Antagonists with high affinity at β1- and β2-adrenoceptors.
↵3-d Have higher intrinsic activity at rodent β3-adrenoceptors than at human β3-adrenoceptors.